JP2016531852A - 非常に強力なグルココルチコイド - Google Patents

非常に強力なグルココルチコイド Download PDF

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Publication number
JP2016531852A
JP2016531852A JP2016516578A JP2016516578A JP2016531852A JP 2016531852 A JP2016531852 A JP 2016531852A JP 2016516578 A JP2016516578 A JP 2016516578A JP 2016516578 A JP2016516578 A JP 2016516578A JP 2016531852 A JP2016531852 A JP 2016531852A
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JP
Japan
Prior art keywords
compound
alkyl
heteroaryl
group
aryl
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JP2016516578A
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Japanese (ja)
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JP2016531852A5 (cg-RX-API-DMAC10.html
Inventor
フアチアン エリック シュー，
フアチアン エリック シュー，
ユアンゼン ヘ，
ユアンゼン ヘ，
カルステン メルシャー，
カルステン メルシャー，
ウェイ イー，
ウェイ イー，
ジンジン シ，
ジンジン シ，
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Shanghai Institute of Materia Medica
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Shanghai Institute of Materia Medica
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Application filed by Shanghai Institute of Materia Medica filed Critical Shanghai Institute of Materia Medica
Publication of JP2016531852A publication Critical patent/JP2016531852A/ja
Publication of JP2016531852A5 publication Critical patent/JP2016531852A5/ja
Pending legal-status Critical Current

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J71/00—Steroids in which the cyclopenta(a)hydrophenanthrene skeleton is condensed with a heterocyclic ring
    • C07J71/0036—Nitrogen-containing hetero ring
    • C07J71/0042—Nitrogen only
    • C07J71/0047—Nitrogen only at position 2(3)
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/10—Anti-acne agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/38—Drugs for disorders of the endocrine system of the suprarenal hormones
    • A61P5/44—Glucocorticosteroids; Drugs increasing or potentiating the activity of glucocorticosteroids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J3/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, substituted in position 17 beta by one carbon atom
    • C07J3/005—Normal steroids containing carbon, hydrogen, halogen or oxygen, substituted in position 17 beta by one carbon atom the carbon atom being part of a carboxylic function
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J5/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane and substituted in position 21 by only one singly bound oxygen atom, i.e. only one oxygen bound to position 21 by a single bond
    • C07J5/0046—Normal steroids containing carbon, hydrogen, halogen or oxygen, substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane and substituted in position 21 by only one singly bound oxygen atom, i.e. only one oxygen bound to position 21 by a single bond substituted in position 17 alfa
    • C07J5/0053—Normal steroids containing carbon, hydrogen, halogen or oxygen, substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane and substituted in position 21 by only one singly bound oxygen atom, i.e. only one oxygen bound to position 21 by a single bond substituted in position 17 alfa not substituted in position 16

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Rheumatology (AREA)
  • Dermatology (AREA)
  • Pulmonology (AREA)
  • Urology & Nephrology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Diabetes (AREA)
  • Endocrinology (AREA)
  • Pain & Pain Management (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)
  • Epidemiology (AREA)
JP2016516578A 2013-09-25 2014-09-25 非常に強力なグルココルチコイド Pending JP2016531852A (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201361882444P 2013-09-25 2013-09-25
US61/882,444 2013-09-25
PCT/US2014/057497 WO2015048316A1 (en) 2013-09-25 2014-09-25 Highly potent glucocorticoids

Publications (2)

Publication Number Publication Date
JP2016531852A true JP2016531852A (ja) 2016-10-13
JP2016531852A5 JP2016531852A5 (cg-RX-API-DMAC10.html) 2017-11-02

Family

ID=52744465

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2016516578A Pending JP2016531852A (ja) 2013-09-25 2014-09-25 非常に強力なグルココルチコイド

Country Status (9)

Country Link
US (1) US9975918B2 (cg-RX-API-DMAC10.html)
EP (1) EP3049089B1 (cg-RX-API-DMAC10.html)
JP (1) JP2016531852A (cg-RX-API-DMAC10.html)
KR (1) KR20160060688A (cg-RX-API-DMAC10.html)
CN (2) CN113845558A (cg-RX-API-DMAC10.html)
AU (1) AU2014324961A1 (cg-RX-API-DMAC10.html)
ES (1) ES2751457T3 (cg-RX-API-DMAC10.html)
HK (1) HK1222565A1 (cg-RX-API-DMAC10.html)
WO (1) WO2015048316A1 (cg-RX-API-DMAC10.html)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2019532071A (ja) * 2016-10-14 2019-11-07 ヴァン アンデル リサーチ インスティテュート 非常に強力な糖質コルチコイドの構造およびデザインのための機構

Families Citing this family (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PT3319611T (pt) 2015-07-06 2021-04-22 Sage Therapeutics Inc Oxisteróis e métodos de utilização dos mesmos
DK3812392T3 (da) 2015-07-06 2025-07-21 Sage Therapeutics Inc Oxysteroler og fremgangsmåder til anvendelse deraf
ES2921010T3 (es) 2016-04-01 2022-08-16 Sage Therapeutics Inc Oxisteroles y procedimientos de uso de los mismos
WO2017193046A1 (en) 2016-05-06 2017-11-09 Sage Therapeutics, Inc. Oxysterols and methods of use thereof
MA46351A (fr) 2016-09-30 2021-06-02 Sage Therapeutics Inc Oxystérols substitués en c7 et procédés en tant que modulateurs nmda
DK3529257T3 (da) 2016-10-18 2023-08-07 Sage Therapeutics Inc Oxysteroler og fremgangsmåder til anvendelse deraf
KR102521573B1 (ko) 2016-10-18 2023-04-14 세이지 테라퓨틱스, 인크. 옥시스테롤 및 그의 사용 방법
WO2021138540A1 (en) 2020-01-03 2021-07-08 Berg Llc Polycyclic amides as ube2k modulators for treating cancer
CN117024499A (zh) * 2023-07-17 2023-11-10 陕西汉江药业集团股份有限公司 在2位引入亚甲基羟基的甾体化合物制备方法
WO2025157225A1 (zh) * 2024-01-24 2025-07-31 浙江柏拉阿图医药科技有限公司 一种高效力糖皮质激素化合物及其制备和用途

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2010114473A1 (en) * 2009-04-03 2010-10-07 Astrazeneca Ab Novel steroidal[3,2-c]pyrazol derivatives with glucocorticoid activity
JP2010540612A (ja) * 2007-10-04 2010-12-24 アストラゼネカ・アクチエボラーグ グルココルチコイド活性を有するステロイド［３，２−ｃ］ピラゾール化合物
JP2012522766A (ja) * 2009-04-03 2012-09-27 アストラゼネカ・アクチエボラーグ グルココルチコイド活性を有するステロイド性［３，２−ｃ］ピラゾール化合物の新規アミド誘導体
JP2012530140A (ja) * 2009-06-16 2012-11-29 メルク・シャープ・アンド・ドーム・コーポレーション グルココルチコイド受容体アゴニストとしての新規［３，２−ｃ］ヘテロアリールステロイド、組成物およびこの使用

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4049813A (en) 1976-07-15 1977-09-20 Sandoz, Inc. Substituted isoxazolo pyridinones
WO2002102807A1 (en) 2001-06-14 2002-12-27 Banyu Pharmaceutical Co., Ltd. Novel isoxazolopyridone derivatives and use thereof
GB0119911D0 (en) 2001-08-15 2001-10-10 Novartis Ag Organic Compounds
US8173670B2 (en) * 2009-01-13 2012-05-08 Van Andel Research Institute Methods of using substituted isoxazolo pyridinones as dissociated glucocorticoids

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2010540612A (ja) * 2007-10-04 2010-12-24 アストラゼネカ・アクチエボラーグ グルココルチコイド活性を有するステロイド［３，２−ｃ］ピラゾール化合物
WO2010114473A1 (en) * 2009-04-03 2010-10-07 Astrazeneca Ab Novel steroidal[3,2-c]pyrazol derivatives with glucocorticoid activity
JP2012522766A (ja) * 2009-04-03 2012-09-27 アストラゼネカ・アクチエボラーグ グルココルチコイド活性を有するステロイド性［３，２−ｃ］ピラゾール化合物の新規アミド誘導体
JP2012530140A (ja) * 2009-06-16 2012-11-29 メルク・シャープ・アンド・ドーム・コーポレーション グルココルチコイド受容体アゴニストとしての新規［３，２−ｃ］ヘテロアリールステロイド、組成物およびこの使用

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2019532071A (ja) * 2016-10-14 2019-11-07 ヴァン アンデル リサーチ インスティテュート 非常に強力な糖質コルチコイドの構造およびデザインのための機構
JP7146750B2 (ja) 2016-10-14 2022-10-04 ヴァン アンデル リサーチ インスティテュート 非常に強力な糖質コルチコイドの構造およびデザインのための機構

Also Published As

Publication number Publication date
EP3049089A4 (en) 2017-08-09
US20160251393A1 (en) 2016-09-01
AU2014324961A8 (en) 2016-04-21
ES2751457T3 (es) 2020-03-31
EP3049089A1 (en) 2016-08-03
AU2014324961A1 (en) 2016-04-14
CN113845558A (zh) 2021-12-28
HK1222565A1 (zh) 2017-07-07
CN105744937A (zh) 2016-07-06
US9975918B2 (en) 2018-05-22
EP3049089B1 (en) 2019-08-21
WO2015048316A1 (en) 2015-04-02
KR20160060688A (ko) 2016-05-30

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